Eliglustat (hemitartrate) (Synonyms: Genz-112638) |
Catalog No.GC43595 |
L'éliglustat (hémitartrate) est un inhibiteur de la glucocérébroside synthase spécifique, puissant et actif par voie orale avec une IC50 de 24 nM.
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Cas No.: 928659-70-5
Sample solution is provided at 25 µL, 10mM.
Eliglustat is a potent and selective inhibitor of glucosylceramide synthase with an IC50 value of 40 nM for the reduction of glucosylceramide synthesis in K562 cells. Inhibition of glucosylceramide synthase, the rate-limiting enzyme in glycosphingolipid synthesis, also reduces production of cell surface gangliosides GM1 and GM3 on K562 and B16/F10 cells, with IC50 values of 24 and 29 nM, respectively. Eliglustat is specific to glucosylceramide synthase over similar enzymes, having minimal activity (IC50 = >10 μM) at α-glucosidase I and II, lysosomal glucocerebrosidase (GBA1), non-lysosomal glucosylceramidase (GBA2), sucrase, and maltase. In vivo, eliglustat induces a dose-dependent decrease in glucosylceramide accumulation in the liver and lungs of D409V/null mice, a model of Gaucher disease. It also prevents further glucosylceramide accumulation if administered after liver and lung deposits have been established.
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